The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101

Author(s): Thomas Mehrling , Yi Chen .

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 16 , Issue 1 , 2016

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Graphical Abstract:


Chemotherapy may still be an essential component to treat cancer in combination with new targeted therapies. But chemotherapy needs to get smarter in order to make those combination regimens more effective and also more tolerable, particularly for an aging population. We describe the first time the synthesis and pharmacological testing of a fusion molecule comprising of the alkylator bendamustine and the HDAC-inhibitor vorinostat. The drug was designed to allow for the exploitation of both mechanisms of action simultaneously with the goal to provide a molecule with superior efficacy over the single agents. The pharmacological testing confirms the full functional capacity of both moieties and encouraging pharmacological data raises the hope that the drug may turn out to be a great addition to the armentarium of anticancer agents.

Keywords: Alkylation, apoptosis, bifunctional, checkpoint arrest, DNA repair, fusion molecule, HDAC inhibition.

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Article Details

Year: 2016
Page: [20 - 28]
Pages: 9
DOI: 10.2174/1871520615666150518092027

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